当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > 8-[18F]fluorooctanoic acid and its beta-substituted derivatives as potential agents for cerebral fatty acid studies: synthesis and biodistribution.

8-[18F]fluorooctanoic acid and its beta-substituted derivatives as potential agents for cerebral fatty acid studies: synthesis and biodistribution.

Abstract：

:Fluorine-18 labeled analogs of 8-fluorooctanoic acid and its structurally modified derivatives with methyl or gem-dimethyl branching or with oxygen substitution at the C3 position were prepared using nucleophilic substitution of the tosylate precursors by [18F]fluoride ion, for evaluation as tracers for cerebral fatty acid metabolism. Tissue distribution studies in rats showed low brain uptakes of these 18F-labeled fatty acid analogs with poor brain-to-blood ratios of activity. The oxygen-substituted analog did not show any significant accumulation of radioactivity in most tissues. The initial brain uptake of activity after injection of ethyl 8-[18F]fluorooctanoate and its free acid remained virtually unchanged over an extended time period, beta-Monomethyl and beta-gem-dimethyl branched analogs had similar brain uptake at the early time period, but they showed rapid clearance of activity from the brain. TLC analysis showed no incorporation of 8-[18F]fluorooctanoic acid and its beta-dimethyl analogs into brain lipids. It was also shown in the metabolite analysis that the labeled metabolites produced from 8-[18F]fluorooctanoic acid are found in blood, and that they could enter the brain to a significant degree. On the contrary, such radioactive metabolites could not be found in the brain in the experiment with the beta-gem-dimethyl branched analog. Thus, the present studies showed that retention of radioactivity in the brain with 8-[18F]fluorooctanoic acid derivatives is mainly attributable to their radioactive metabolites, and that the rapid clearance of beta-branched analogs from the brain is due to the lack of availability as substrates in the cerebral fatty acid metabolism.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Nagatsugi F,Sasaki S,Maeda M

doi

10.1016/0969-8051(94)90160-0

subject

Has Abstract

pub_date

1994-08-01 00:00:00

pages

809-17

issue

6

eissn

0969-8051

issn

1872-9614

pii

0969-8051(94)90160-0

journal_volume

21

pub_type

杂志文章

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